N-ARYL-4-(5-NITROFURAN-2-YL)-PYRIMIDINE-5-AMINES WITH ANTIBACTERIAL ACTIVITY AND METHOD FOR THEIR OBTAINING Russian patent published in 2018 - IPC C07D405/04 A61K31/345 A61K31/506 A61P31/04 

FIELD: pharmacology.

SUBSTANCE: invention relates to new N-aryl-4-(5-nitrofuran-2-yl)-pyrimidine-5-amines of general formula I , where a: R¹=R²=R³=H; b: R²=CH₃, R¹=R³=H; c: R²= OCH₃, R¹=R³=H; d: R¹=R²=R³=OCH₃ and a method for their preparation, in which 5-bromo-4-(5-nitrofuran-2-yl)pyrimidine (6) is mixed with the corresponding arylamine taken in 1.5 times excess, palladium (II) acetate and 1,1'-bis (diphenylphosphino)ferracene taken in catalytic amounts and potassium phosphate taken in 2.5-fold excess, the resulting mixture is dissolved in degassed 1,4-dioxane and heated at 85°C with vigorous stirring for at least 15 hours, followed by solvent distillation on a rotary evaporator under reduced pressure, and the resulting residue is subjected to chromatographic separation on a silica gel column with a ratio of ethyl acetate: hexane components of 1:3 in the eluent.

EFFECT: highly effective method is proposed for the preparation of a compound that has a broad spectrum of antibacterial activity against coccal infections caused by gonococci or staphylococcus aureus, as well as purulent inflammatory infectious diseases of skin and mucous membranes caused by staphylococci and streptococci.

2 cl, 1 tbl, 4 ex